Invitro Comparative Analysis of the Flexural Strength of 4 Different Commercially Available Provisional Materials Used in Fixed Partial Dentures – An Original Research

Background: Provisional Prosthesis in fixed partial dentures are subjected to Flexure under stress. Selection of appropriate material for fabrication of Provisional is of utmost importance as the Provisional prosthesis has to remain in function till definitive prosthesis is delivered. Material & Methods: Bar type specimens of four different commercially available brands for provisional restorations fabricated according to ADA specification No. 27 and immersed in artificial saliva. The specimens were fractured under 3-point loading test. Results: The flexural strength ranged between 60 to 110 Mpa. BisGMA Auto polymerizing composite resin from Dentsply Caulk shows the highest flexural strength. Conclusion: Within the limitations of this study, the flexural strengths were material specific rather than category one. The BisGMA composite based resin shows significantly higher flexural strength over other materials

Enzymatic properties and degradation characterization of a bis(2-hydroxyethyl) terephthalate hydrolase from Saccharothrix sp / 生物工程学报

The discovery of new enzymes for poly(ethylene terephthalate) (PET) degradation has been a hot topic of research globally. Bis-(2-hydroxyethyl) terephthalate (BHET) is an intermediate compound in the degradation of PET and competes with PET for the substrate binding site of the PET-degrading enzyme, thereby inhibiting further degradation of PET. Discovery of new BHET degradation enzymes may contribute to improving the degradation efficiency of PET. In this paper, we discovered a hydrolase gene sle (ID: CP064192.1, 5085270-5086049) from Saccharothrix luteola, which can hydrolyze BHET into mono-(2-hydroxyethyl) terephthalate (MHET) and terephthalic acid (TPA). BHET hydrolase (Sle) was heterologously expressed in Escherichia coli using a recombinant plasmid, and the highest protein expression was achieved at a final concentration of 0.4 mmol/L of isopropyl-β-d-thiogalactoside (IPTG), an induction duration of 12 h and an induction temperature of 20 ℃. The recombinant Sle was purified by nickel affinity chromatography, anion exchange chromatography, and gel filtration chromatography, and its enzymatic properties were also characterized. The optimum temperature and pH of Sle were 35 ℃ and 8.0, and more than 80% of the enzyme activity could be maintained in the range of 25-35 ℃ and pH 7.0-9.0 and Co2+ could improve the enzyme activity. Sle belongs to the dienelactone hydrolase (DLH) superfamily and possesses the typical catalytic triad of the family, and the predicted catalytic sites are S129, D175, and H207. Finally, the enzyme was identified as a BHET degrading enzyme by high performance liquid chromatography (HPLC). This study provides a new enzyme resource for the efficient enzymatic degradation of PET plastics.

Expression, purification and characterization of a novel bis (hydroxyethyl) terephthalate hydrolase from Hydrogenobacter thermophilus / 生物工程学报

PET (polyethylene terephthalate) is one of the most important petrochemicals that is widely used in mineral water bottles, food and beverage packaging and textile industry. Because of its stability under environmental conditions, the massive amount of PET wastes caused serious environmental pollution. The use of enzymes to depolymerize PET wastes and upcycling is one of the important directions for plastics pollution control, among which the key is the depolymerization efficiency of PET by PET hydrolase. BHET (bis(hydroxyethyl) terephthalate) is the main intermediate of PET hydrolysis, its accumulation can hinder the degradation efficiency of PET hydrolase significantly, and the synergistic use of PET hydrolase and BHET hydrolase can improve the PET hydrolysis efficiency. In this study, a dienolactone hydrolase from Hydrogenobacter thermophilus which can degrade BHET (HtBHETase) was identified. After heterologous expression in Escherichia coli and purification, the enzymatic properties of HtBHETase were studied. HtBHETase shows higher catalytic activity towards esters with short carbon chains such as p-nitrophenol acetate. The optimal pH and temperature of the reaction with BHET were 5.0 and 55 ℃, respectively. HtBHETase exhibited excellent thermostability, and retained over 80% residual activity after treatment at 80 ℃ for 1 hour. These results indicate that HtBHETase has potential in biological PET depolymerization, which may facilitate the enzymatic degradation of PET.

Bis (2-butoxyethyl) Phthalate Delays Puberty Onset by Increasing Oxidative Stress and Apoptosis in Leydig Cells in Rats / 生物医学与环境科学（英文）

OBJECTIVE@#This study investigated the effects of bis (2-butoxyethyl) phthalate (BBOP) on the onset of male puberty by affecting Leydig cell development in rats.@*METHODS@#Thirty 35-day-old male Sprague-Dawley rats were randomly allocated to five groups mg/kg bw per day that were gavaged for 21 days with BBOP at 0, 10, 100, 250, or 500 mg/kg bw per day. The hormone profiles; Leydig cell morphological metrics; mRNA and protein levels; oxidative stress; and AKT, mTOR, ERK1/2, and GSK3β pathways were assessed.@*RESULTS@#BBOP at 250 and/or 500 mg/kg bw per day decreased serum testosterone, luteinizing hormone, and follicle-stimulating hormone levels mg/kg bw per day (P < 0.05). BBOP at 500 mg/kg bw per day decreased Leydig cell number mg/kg bw per day and downregulated Cyp11a1, Insl3, Hsd11b1, and Dhh in the testes, and Lhb and Fshb mRNAs in the pituitary gland (P < 0.05). The malondialdehyde content in the testis significantly increased, while Sod1 and Sod2 mRNAs were markedly down-regulated, by BBOP treatment at 250-500 mg/kg bw per day (P < 0.05). Furthermore, BBOP at 500 mg/kg bw per day decreased AKT1/AKT2, mTOR, and ERK1/2 phosphorylation, and GSK3β and SIRT1 levels mg/kg bw per day (P < 0.05). Finally, BBOP at 100 or 500 μmol/L induced ROS and apoptosis in Leydig cells after 24 h of treatment in vitro (P < 0.05).@*CONCLUSION@#BBOP delays puberty onset by increasing oxidative stress and apoptosis in Leydig cells in rats.@*UNLABELLED@#The graphical abstract is available on the website www.besjournal.com.

Phytochemical, Antioxidant, Antibacterial and Antifungal Investigations of Thuja orientalis Cone

Background of the Study: Thuja orientalis L. is an indigenous medicinal plant belonging to family Cupressaceae found in Darjeeling Himalayan region, Dooars and Tarai region of India. The plant cone has been used traditionally as medicine to treat various diseases, like bronchitis, bacterial skin infection, osteoarthritis, trigeminal neuralgia. Aim: The aim of the present study is to evaluate the plant cone for phytochemical constinuents, and in vitro antioxidant, and antimicrobial properties. Place and Duration of Study: All the experiments were done in the Department of Biotechnology, University of North Bengal, Darjeeling, West Bengal, 734013, India. Methodology: Methanolic extract of T. orientalis cone was analyzed for phytochemicals by various biochemical methods. Antioxidant properties were analyzed by in vitro assays of DPPH, ABTS, NO and H2O2 scavenging. Antibacterial property was analyzed by agar well diffusion method and antifungal assay was monitored by radial growth bioassay. Results: Methanolic extract of T. orientalis cone contained flavonoid, phenol, saponin, tannin, terpenoid and alkaloid. The extract showed significant in-vitro antioxidant and antimicrobial activity. Conclusions: The study revealed that T. orientalis cone has potential as source of antioxidant, antibacterial and antifungal agents. Our further study is directed towards the isolation, and characterization of active compound from methanolic extract and evaluation of its potentiality against high blood sugar.

Specific antitumor activity and mechanism of protonic bis-phenanthroline / 药学学报

Hepatocellular carcinoma (HCC) is a common malignant tumor worldwise. The incidence rate of HCC is high and is easy to metastasis and recurrence, which seriously affects human health. Traditional chemical drugs have some challenges such as toxicity, side effects, and multidrug resistance, thus it is urgent to find new drugs and effective targets. Here we synthesized a novel chemical, protonic bis-phenanthroline (H-BP), and the antitumor effect was investigated in the study. The results showed that H-BP could selectively inhibit the proliferation of tumor cells and cause HCC apoptosis. And also, in HCC tumor-bearing mice, H-BP could effectively prevent the growth of tumor mass, even completely eliminate the tumor at medium dose (5 mg·kg-1) and high dose (10 mg·kg-1), and meanwhile H-BP has no significant effect on the body weight of mice. The experimental protocol was approved by the Animal Ethics Committee of Southwest University, and the experimental operation was strictly carried out in accordance with the ethical principles of animal use and care. Mechanism studies showed that H-BP induced HCC apoptosis was related to down-regulation the expression of pleomorphic adenoma gene like-2 (PLAGL2), a oncogene transcription factor, resulting in the down-regulation of PLAGL2 downstream proteins hypoxia inducible factor and β-catenin. This study not only introduces the dimerization method to form novel compounds that will provide a new approach for drug design, but also suggests that PLAGL2 may be an effective target in tumor therapy.

Color and surface gloss stability of bis-acryl and resin composite after exposure to cigarette smoke / Estabilidade de cor e brilho superficial de resinas compostas e bisacrílicas após exposição por fumaça de cigarro

Objective: To evaluate color and surface gloss stability of bis-acryl resins and resin composites, submitted to artificial staining with cigarette smoke. Material and Methods: Specimens of each material were prepared (n=15). Two resin composites (GrandioSO [RCG], Filtek Supreme [RCZ]) and five bis-acryl resins (Luxatemp Star [BisLUX], Protemp4 [BisPRO], Structor3 [BisSTR], Visalys Temp [BisVIS] and Yprov [BisYPR]) were tested. Initial color was assessed using a spectrophotometer and surface gloss with a glossmeter. Samples were submitted to smoke exposure (10 cigarettes under 8 minutes per cycle). After 3 and 6 cycles, color and gloss were reassessed. Final readings were performed after brush prophylaxis. Data were analyzed using two-way repeated ANOVA and Tukey's test (p<0.05). Results: Differences and interaction of factors (p<0.01) were detected for both color and gloss readings. Resin composites were the least affected by aging, with gloss reduction after prophylaxis. Differences were detected among bis-acryl resins, with better results for BisLUX and BisPRO. BisPRO and BisSTR, showed reduction in gloss after 60 cigarettes, while BisYPR gloss decreased at all evaluated periods. Conclusion: Resin composites are less susceptible to changes after smoke exposure, while bis-acryl resins results are brand-dependent. Prophylaxis negatively influenced the surface gloss of most of the tested materials (AU)

Objetivo: Avaliar a estabilidade de cor e brilho superficial de resinas compostas e bisacrílicas, submetidos ao manchamento artificial por fumaça de cigarro. Material e Métodos: Foram preparados espécimes de cada material (n=15). Duas resinas compostas (GrandioSO [RCG], Filtek Supreme [RCZ]) e cinco resinas bisacrílicas (Luxatemp Star [BisLUX], Protemp4 [BisPRO], Structor3 [BisSTR], Visalys Temp [BisVIS] e Yprov [BisYPR]) foram testados. A cor inicial foi avaliada usando um espectrofotômetro e o brilho de superfície com um medidor de brilho. As amostras foram submetidas à exposição de fumaça de cigarro (10 cigarros com até 8 minutos por ciclo). Após 3 e 6 ciclos, a cor e o brilho foram reavaliados. As leituras finais foram realizadas após a profilaxia escova de robinson. Os dados foram analisados usando de medidas repetidas e teste de Tukey (p<0,05). Resultados: Foram detectadas diferenças e interação de fatores (p<0,01) tanto para leituras de cor quanto para leituras de brilho. As resinas compostas foram as menos afetados pelo envelhecimento, com redução do brilho após a profilaxia. Foram detectadas diferenças entre as resinas bisacrílicas, com melhores resultados para BisLUX e BisPRO. BisPRO e BisSTR, mostraram redução de brilho após 60 cigarros, enquanto que o brilho da BisYPR diminuiu em todos os períodos avaliados. Conclusão: As resinas compostas são as menos suscetíveis a mudanças após a exposição à fumaça, enquanto os resultados das resinas bisacrílicas são dependentes da marca. A profilaxia influenciou negativamente o brilho de superfície da maioria dos materiais testados.(AU)

Impacto de la anestesia intravenosa en cirugía robótica para paciente de alto riesgo sometido a cirugía oncológica de larga duración en el Centro Médico Naval / Impact of intravenous anesthesia in robotic surgery for high-risk patient undergoing long-term oncologic surgery at the Naval Medical Center

Resumen: La práctica de cirugía robótica es un proceso complejo que implica desarrollo y tecnología no sólo en el campo de la cirugía, sino también en el campo de la anestesiología. Implica un proceso multifactorial, ya que ha generado un cambio drástico multidisciplinario basado en tecnología de punta que pretende ofrecer mejores condiciones durante el manejo perioperatorio en cirugía robótica. La anestesia total intravenosa cumple objetivos específicos en relación a la posición del paciente, relajación cerebral, neuroprotección, hemodinamia, pérdida y recuperación de la conciencia, parálisis neuromuscular, parámetros ventilatorios, etc. Ofrece seguridad y calidad al paciente durante el procedimiento con una mínima interferencia con el monitoreo electrofisiológico y permite modular la profundidad anestésica desde una neurosedación hasta una anestesia general, de acuerdo a las diferentes etapas de la cirugía. Un factor atribuible a la anestesia moderna para el éxito de la cirugía robótica es usar diferentes agentes anestésicos que promuevan inducción, mantenimiento y emersión anestésica más rápida y suave, a fin de reducir el tiempo de recuperación del estado de conciencia, funciones básicas y psicomotoras como la anestesia general multimodal.

Abstract: The practice of robotic surgery is a complex process, involving development and technology; not only in the surgery field but also in the anesthesiology field. It implies a multifactorial process since it has generated a drastic multidisciplinary change based on state-of-the-art technology; which aims to offer better conditions during perioperative management in robotic surgery. Intravenous Total Anesthesia accomplishes specific objectives in relation to patient position, brain relaxation, neuroprotection, hemodynamics, loss and recovery of consciousness, neuromuscular paralysis, ventilatory parameters, providing safety and quality during the procedure; with minimal intervention during electrophysiological monitoring and enabling anesthetic depth to be modulated from neurosedation to general anesthesia, according to the different stages of the surgery. A factor attributable to modern anesthesia for robotic surgery success is to employ different anesthetic agents promoting induction, maintenance of general anesthesia, smother and faster anesthetic emersion, for the purpose of reducing recovery time of the state of consciousness), basic and psychomotor functions; as is the general multimodal anesthesia.

Determination of bis(2-chloroethyl)amine hydrochloride and 1-(3-chloropropyl)-4-(3-chlorophenyl)piperazine hydrochloride in trazodone hydrochloride by UPLC-MS/MS / 药学学报

An UPLC-MS/MS method was established for the quantification of the genotoxic impurities bis(2-chloroethyl)amine hydrochloride and 1-(3-chloropropyl)-4-(3-chlorophenyl)piperazine hydrochloride in trazodone hydrochloride. The chromatographic separation of the two genotoxic impurities was performed on Waters ACQUITY UPLC BEH C18 column (100 mm×2.1 mm, 1.7 μm) at 20 ℃. A mixture of 5 mmol·L-1 ammonium hydrogen carbonate aqueous solution and acetonitrile at a flow rate of 0.3 mL·min-1 in gradient elution mode was employed as mobile phase. The UPLC-MS/MS was equipped with electrospray ionization in positive ionization mode and adopted multiple reaction monitoring mode. We found that the calibration curves of the two genotoxic impurities were linear in the range of 0.1-10 ng·mL-1. The limit of detection was 0.10 ng·mL-1 for bis(2-chloroethyl)amine hydrochloride and the average recovery was 101.53% (RSD = 4.06%). The limit of detection was 0.01 ng·mL-1 for 1-(3-chloropropyl)-4-(3-chlorophenyl)piperazine hydrochloride and the average recovery was 97.95% (RSD = 1.27%). The sample solution was stable for 24 h. No bis(2-chloroethyl)amine hydrochloride was detected in the samples, and the content of 1-(3-chloropropyl)-4-(3-chlorophenyl)piperazine hydrochloride in the samples was within the limit. This research provides a method to improve the quality control standards of trazadone.

Pró-Fármacos dendriméricos potencialmente ativos em Malária e Tuberculose: Síntese e avaliação da atividade biológica / Dendrimeric prodrugs potentially active in malaria and tuberculosis: Synthesis and evaluation of biological activity

HIV/AIDS, tuberculose, malária e as doenças tropicais negligenciadas representam uma grande preocupação em Saúde em muitas regiões do mundo. Os fármacos disponíveis para o tratamento apresentam diversos problemas, tais como toxicidade e resistência ao parasita. Mesmo com esse triste panorama, o investimento em pesquisa nessa área é, ainda, pouco significativo. Assim, dentre os métodos de modificação molecular para melhorar propriedades farmacêuticas, farmacocinéticas e/ou farmacodinâmica de compostos bioativos destaca-se a latenciação. Já os dendrímeros vêm despertando interesse em aplicações biológicas, principalmente como transportadores de fármacos, além de atuarem como transportadores de genes, imagem em diagnóstico e compostos com ação per se. Face ao exposto e tendo em vista o caráter promissor dos dendrímeros como sistemas de drug delivery, o objetivo deste trabalho foi a síntese de pró-fármacos dendriméricos potencialmente ativos em malária e tuberculose. Os dendrímeros de Bis-MPA (gerações 0, 1 e 2) foram sintetizados pelo grupo do Professor Scott Grayson, da Tulane University (EUA). No Brasil, foram feitas as funcionalizações destes compostos, através do acoplamento do ácido succínico (que funciona como espaçante) e as moléculas ativas. Selecionaram-se as seguintes substâncias: (1) primaquina, com ação antimalárica e (2) isoniazida, de ação nos primeiros estágios da tuberculose. Foram sintetizados os pró-fármacos dendriméricos de isoniazida nas gerações 0 e 1 (G0-Iso e G1-Iso), e primaquina nas gerações 0, 1 e 2 (G0-Pq, G1-Pq e G2Pq). Importante mencionar que os resultados de Ressonância Magnética e Nuclear de 1H e de 13C demostraram as obtenções dos respectivos produtos, porém contendo impurezas. Já a análise do resultado proveniente da espectrometria de massas do composto G0-Iso revelou a presença de um subproduto ciclizado da isonizaida succinoilada (CIso-Suc), o qual pode ser um potencial pró-fármaco ou apresentar atividade per se. Como não se conhece este composto, o laboratório coordenado pela Profas Elizabeth Igne Ferreira e Jeanine Giarolla manifestou interesse em pesquisa-lo, principalmente quanto suas propriedades físico- químicas, bem como quanto à atividade biológica. Assim, utilizando metodologia analítica previamente estabelecida para o G0-Iso, os estudos de estabilidade química da CIso-Suc, em diferentes valores de pH, demonstraram a capacidade da forma ciclizada em se converter no protótipo Iso-Suc, majoritariamente em pH 7,4 e 8,5. Como perspectivas, destaca-se a avaliação da estabilidade enzimática deste potencial derivado. Ressalta-se, ainda, a a avaliação da respectiva atividade antimicobacteriana. Em relação aos pró-fármacos, as necessidades de aprimoramentos das sínteses são, também, evidenciadas. Uma vez sintetizados e caracterizados, estes últimos derivados serão avaliados quanto à atividade biológica. Ademais, estudos computacionais, sobretudo simulações de docking molecular, foram desenvolvidos com intuito de se entender o modo de interação de alguns compostos com alvos biológicos pré-determinados

HIV/AIDS, tuberculosis, malaria and neglected diseases are a major health concern in many regions of the world. The drugs available present various problems, such as toxicity and parasite resistance. Even with this sad outlook, research investment in this area is still insignificant. Among the molecular modification methods to improve the pharmaceutical, pharmacokinetic and/or pharmacodynamic properties we stands out prodrug design. On the other hand, dendrimers are arousing interest in biological applications, mainly as drug carriers, besides gene delivery, diagnostic imaging, as well as acting as compounds with activity per se. Considering that, added to the promising dendrimer drug delivery features, the aim of this study was to synthesize potentially active dendrimer prodrugs in malaria and tuberculosis. Bis-MPA dendrimers (generations 0, 1 and 2) were synthesized by the group of Professor Scott Grayson of Tulane University (USA). Herein in Brazil, the compounds were functionalized by coupling succinic acid (spacer group), as well as the active molecules. We selected the following substances: (1) primaquine, with antimalarial action and (2) isoniazid, acting in the early stages of tuberculosis. Isoniazid dendrimer prodrugs were synthesized generations 0 and 1 (G0-Iso and G1-Iso), and primaquine in generations 0, 1 and 2 (G0-Pq, G1-Pq and G2-Pq). It is important to mention that the results related to Nuclear and Magnetic Resonance 113C showed chemical structures features, however with impurities. Analysis of the mass spectrometry regarding G0-Iso has revealed the presence of a cyclized by-product of succinylated isonized (CIso-Suc), which may be a potential prodrug or may presentactivity itself. Using the analytical methodology performed for G0-Iso, ICso-Suc demonstrated its ability to convert the Iso-Suc prototype at different pH values, especially at pH 7.4 and 8.5. As perspectives, we highlight the determinations of the chemical stability of ICsoSuc at pH 1.5 and 6.0, as well as the evaluation of the enzymatic stability. We will also investigate the respective antimicobacterial activities. Regarding prodrugs, the needs for synthesis enhancements are also necessary. Once synthesized and characterized, these latter derivatives will be evaluated for biological activity. Moreover, computational studies, especially molecular docking simulations, were developed in order to understand the mode of interaction of some compounds with predetermined biological targets

Selective activity of diselenides against Aedes aegypti (Diptera: Culicidae) larvae

Abstract INTRODUCTION: Aedes aegypti (L.) is the major vector of arboviruses that causes serious public health concerns in tropical and subtropical countries. METHODS: We examined the larvicidal activity of 1,2-diphenyldiselenide [(PhSe)2] and 1,2-bis(4-chlorophenyl) diselenide [(p-ClPhSe)2] and determine its toxicity to different non-target organisms. RESULTS: (PhSe)2 and (p-ClPhSe)2 killed Ae. aegypti L3 larvae with LC50/24h values of 65.63 µM (20.48 mg/L) and 355.19 µM (135.33 mg/L), respectively. (PhSe)2 was not toxic to the four model organisms. CONCLUSIONS: (PhSe)2 is a larvicidal compound with selective action against Ae. aegypti larvae. The mechanisms of action of (PhSe)2 under field conditions remain to be investigated.

Crude extract of the tropical tree Gallesia integrifolia (Phytolaccaceae) for the control of Aedes aegypti (Diptera: Culicidae) larvae / Extracto crudo del árbol tropical Gallesia integrifolia (Phytolaccaceae) para el control de larvas de Aedes aegypti (Diptera: Culicidae)

Introduction: Phytoinsecticides are alternatives to control insects in different stages, Gallesia integrifolia (Spreng.) Harms, Phytolacaceae family, popularly known as pau d'alho, garlic tree, and guararema in Brazil, is known due to its strong alliaceous odor because of the presence of sulfur molecules in the plant. This species presents biological activity and potential insecticide effect that is still unexploited. Objective: This study aimed to evaluate the biological activity of the ethanolic crude extract from G. integrifolia leaves, flowers, and fruits on the control of Aedes aegypti third-stage larvae and pupae. Methods: The botanical material was collected in city Umuarama, Paraná, Brazil at the coordinates (23º46'16" S & 53º19'38" WO), and altitude of 442 m, the fruits of G. integrifolia were collected in May and the leaves and flowers in December 2017. The crude extracts of G. integrifolia leaves, flowers, and fruits were prepared by dynamic maceration technique. The chemical composition of the extracts was determined by gas chromatography coupled to a mass spectrometry. The insecticidal activity of the crude extracts of G. integrifolia were carried out on larvae and pupae of A. aegypti in concentrations between 0.001 to 25 000 mg/mL, and afterwards the lethal concentrations that kill 50 % (LC50) and 99.9 % (LC99.9) were determined by probit analysis. Anticholinesterase activity was determined by bioautographic method at concentrations from 0.000095 to 50 mg/mL. Results: The yield of G. integrifolia crude extracts were 8.2, 9.1, and 17.3 % for flowers, fruits, and leaves, respectively. The chemical composition of G. integrifolia extracts was characterized by presence of fatty acid esters, phytosterols, vitamins, oxygenated diterpenes and organosulfur compounds. The flower extract presented the high amount of sulfur compounds (20.2 %) such as disulfide, bis (2-sulfhydryl ethyl) (11.9 %), 2,3,5-trithiahexane (6.2 %), 1,2,4-trithiolane (1.1 %), and 2,4-dithiapentane (1.1 %). Regarding the insecticidal activity, flower extract showed highly active with LC99.9 of 0.032 mg/mL and LC99.9 of 0.969 mg/mL on A. aegypti larvae and pupae, respectively, and the highest inhibition of acetylcholinesterase enzyme (0.00019 mg/mL) ex situ. The flower extract presented anticholinesterase and larvicide activity, respectively, 12.8 % and 35.6 % greater than the control temephos. Conclusions: This study opens new perspectives on the use of extracts from G. integrifolia as a bioinsecticide alternative for the control of A. aegypti larvae and pupae.

Introducción: Los fitoinsecticidas son alternativas para el control de insectos en diferentes etapas, Gallesia integrifolia (Spreng.) Harms, familia Phytolacaceae, conocida popularmente como pau d'alho, árbol de ajo y guararema en Brasil, es conocida por su fuerte olor aliáceo debido a la presencia de moléculas de azufre en la planta. Esta especie presenta actividad biológica y potencial efecto insecticida que aún no está explotado. Objetivo: El objetivo de este estudio fue evaluar la actividad biológica del extracto crudo etanólico de las hojas, flores y frutos de G. integrifolia en el control de las larvas y pupas de la tercera etapa de Aedes aegypti. Métodos: El material botánico fue recolectado en la ciudad de Umuarama, Paraná, Brasil (23º46'16" S & 53º19'38" W), a una altitud de 442 m y los frutos de G. integrifolia fueron recolectados en mayo de 2017 y las hojas y flores en diciembre del mismo año. Los extractos crudos de hojas, flores y frutos de G. integrifolia se prepararon por técnica de maceración dinámica. La composición química de los extractos se determinó por cromatografía de gases acoplada a espectrometría de masas. La actividad insecticida de los extractos crudos de G. integrifolia fue evaluada en larvas y pupas de A. aegypti en concentraciones entre 0.001 a 25 000 mg/mL, y las concentraciones letales que matan 50 % (CL50) y 99.9 % (CL99.9) de larvas fueron determinados por análisis de probit. La actividad anticolinesterasa fue evaluada por método bioautográfico en concentraciones de 0.000095 a 50 mg/mL. Resultados: El rendimiento de los extractos crudos de G. integrifolia fue de 8.2, 9.1 y 17.3 % para flores, frutos y hojas, respectivamente. La composición química de los extractos de G. integrifolia se caracterizó por la presencia de ésteres de ácidos grasos, fitosteroles, vitaminas, diterpenos oxigenados y compuestos organosulfurados. El extracto de las flores presentó alta cantidad de compuestos de azufre (20.2 %) como disulfuro, bis(2-sulfhidril etilo) (11.9 %), 2,3,5-tritiahexano (6.2 %), 1,2,4-tritiolano (1.1 %) y 2,4-ditiapentano (1.1 %). En relación con la actividad insecticida, el extracto de las flores mostró una gran actividad con CL99.9 de 0.032 mg/mL y CL99.9 de 0.969 mg/mL en larvas y pupas de A. aegypti, respectivamente, y la inhibición más alta de la enzima acetilcolinesterasa (0.00019 mg/mL) ex situ. El extracto de las flores presentó actividad anticolinesterasa y larvicida, 12.8 y 35.6 %, respectivamente, mayor que el control temephos. Conclusiones: Este estudio abre nuevas perspectivas sobre el uso de extractos de G. integrifolia como alternativa bioinsecticida para el control de larvas y pupas de A. aegypti.

Contaminação em larga escala por Bisfenol-A: estamos conscientes do risco e formas de exposição? / Large-scale contamination by Bisphenol A: are we aware of the risk and forms of exposure?

Resumo O Bisfenol-A (BFA) é uma substância amplamente empregada no cotidiano, principalmente nos materiais plásticos. Este estudo avaliou a exposição de universitários ao disruptor endócrino BFA, o conhecimento dos mesmos acerca dessa substância e dos seus danos à saúde humana. Trata-se de um estudo transversal descritivo realizado com 500 estudantes de uma Universidade de Curitiba. A amostra foi selecionada de forma proporcional as três grandes áreas do conhecimento, sendo que os cursos entrevistados foram sorteados. Aos estudantes aplicou-se um questionário objetivo composto por três partes: socioeconômica, avaliação da exposição e testes de conhecimento. Dos respondentes, 91,3% consomem alimentos armazenados em embalagens plásticas, 90,06% utilizam bebidas nesse tipo de recipiente e 84,8% consomem bebidas/alimentos enlatados. Entretanto, apenas 19,8% já ouviram falar em BFA e 97,2% não sabem sobre a relação entre a exposição ao BFA e alterações endócrinas. Observou-se uma alta taxa de exposição ao BFA e um baixo nível de conhecimento sobre o assunto. Essa desproporção evidencia a necessidade de pesquisas mais aprofundadas sobre o tema na população brasileira, além da ampliação de medidas informativas.

Abstract Bisphenol A (BPA) is a substance extensively used in daily life, mainly in plastic materials. This study assessed the exposure of university students to endocrine disruptor BPA, their knowledge about this substance and the damage it causes to human health. This is a cross-sectional descriptive study carried out with 500 students from a University in Curitiba. The sample was selected proportionally to the three major areas of knowledge, and the courses interviewed were drawn at random. Students were asked to fill out an objective questionnaire consisting of three parts: socioeconomic, assessment of exposure and knowledge tests. Of the respondents, 91.3% consume food stored in plastic packaging, 90.06% use drinks in this type of container and 84.8% consume canned food/drinks. However, only 19.8% have heard of BPA and 97.2% do not know about the relationship between exposure to BPA and endocrine changes. A high rate of exposure to BPA and a low level of knowledge on the subject was detected. This disproportion highlights the need for more in-depth research on the topic among the Brazilian population, in addition to broadening dissemination of information measures on the issue.

Influence of Different Surface Treatments on the Bond Strength Between Composites and Resin Cement / INFLUÊNCIA DE DIFERENTES TRATAMENTOS DE SUPERFÍCIE NA RESISTÊNCIA DE UNIÃO ENTRE COMPÓSITOS E CIMENTO RESINOSO

The aim of this study was to evaluate the influence of different surface treatments on bond strength (BS) between composite and a resin cement trough microshear bond strength test. Seventy five discs (10x2 mm) of Filtek P90, Filtek Z250 and Filtek Z350 XT (3M ESPE), were divided into 5 groups according to the treatment: C= control - no treatment; sandblasting J= aluminum oxide (50µm); sandblasting JE = + 99.3% ethanol for 5 min; silica coating S = (3M-ESPE Cojet - 30 microns); SS = silica coating + silane. PVC tubes (0.5 x 0.80 mm) were attached on the composite disc, and then, inserted resin cement (3M ESPE-RelyX ARC). After 24 hours artificial saliva storage at 37oC, the specimens were tested for microshear crosshead speed of 1.0 mm/min. Data were evaluated in two-way ANOVA and Tukey's test (5%) for contrast. The results showed that sandblasting with aluminum oxide (J) was efficient in increasing the BS for composites Z350 and P90. For the Z250, there were no difference between treatments. Also, CS showed results similar to controls for all composites. SE showed the worst results for Z350 e P90. BS values were dependent on the type of composite and the surface treatment used. Sandblasting with aluminum oxide seems to be an effective surface treatment for composites and may lead to higher BS values, while the use of ethanol could be harmful.

O objetivo deste estudo foi avaliar a influência de tratamentos de superfície na resistência de união (RU) entre compósitos e um cimento resinoso. Setenta e cinco discos (10x2 mm) das resinas Filtek P90, Filtek Z250 e Filtek Z350 (3M ESPE) foram divididos em 5 grupos de acordo com o tratamento: N= sem tratamento; S= jateamento com óxido de alumínio (50µm); SE= jateamento de óxido de alumínio + 99,3% de etanol por 5 min; C= jateamento de sílica com Cojet - 30 microns (3M ESPE); CS= jateamento de sílica + silano. Tubos de PVC (0,5 x 0,80 mm) foram fixados nos discos e o cimento resinoso (RelyX ARC, 3M ESPE) foi inserido. Após 24 horas de armazenamento em saliva artificial a 37oC, os espécimes foram submetidos ao teste de microcisalhamento com velocidade de 1,0 mm/min. Os dados foram avaliados em ANOVA de dois fatores e no teste de Tukey (5%) para contraste. Os resultados mostraram que o tratamento com oxido de alumínio (J) foi eficiente no aumento da RU nos compósitos Filtek Z350 e P90. Não houve diferença entre tratamentos para a Z250. Grupo CS mostrou resultados semelhantes aos do controle para todos os compósitos. Já o SE mostrou os piores resultados de RU. Concluiu-se que os valores de RU foram dependentes do tipo de compósito e do tratamento de superfície utilizado. O jateamento com óxido de alumínio parece ser um tratamento de superfície eficaz e pode elevar os valores de RU, já o uso de etanol pode ser prejudicial

Molecular Docking Studies Of Hgv-6 Analogue As A Potential Pbp-1a Inhibitor

Objective: The sygnificance of this study is to find a new hexagamavunon-6 analogue (HGV-6); 3,5-bis-(4´-chlorobenzylidene)-tetrahydro-4H-thiopyran-4-one (D144); 3,5-bis-(2´,4´-dichlorobenzylidene)-tetrahydro-4H-thiopyran-4-one (D154); 3,5-bis-(3´,5´-dichlor ro-4´-hydroxybenzylidene)-tetrahydro-4H-thiopyran-4-one (D156) as a potential PBP-1A inhibitor. Methods: Docking method through Molecular Operating Environment (MOE) software was used to design a new HGV-6 analogue and study its interaction with penicillin binding protein (PBP-1a). This docking study used parameterized model 3 (PM3) method through Polak Ribiere algorithm to calculate the optimal structural geometry of the compound. Protein validation was carried out to ensure that the protein was suitable for use. Results: The results of the docking study show that the docking scores of D144 (-9.7942) and D154 (-10.1961) are higher than D156 (-12.2604), while D156 is lower than HGV-6 (-11.7958). Ampicillin (-13.6496) as a native ligand has the smallest docking score compared to the test compounds. Conclusion: The results of the docking study show that 3,5-bis-(3,5-dichloro-4-hydroxybenzylidene)-tetrahydro-4H-thiopyran-4-one (D156) has a better potential antibacterial compound than HGV-6.

Influence of Bispectral Index Monitoring on Isoflurane Minimum Alveolar Concentration in Off Pump Cardiac Surgeries

Off pump CABG is the most commonly performed cardiac surgical procedure involving multi vessel grafting through median sternotomy. Approach of lateral and posterior walls of heart for grafting, necessitates need for lifting or tilting heart producing elevated atrial pressures, fall in cardiac output and thus profound hypotension. Maintaining delicate balance between myocardial oxygen demand and supply is crucial to prevent myocardial insults and associated sequelae for which the mean arterial pressure is maintained >70 mmHg to facilitate adequate coronary perfusion pressure achieved by infusion of vasopressors like dobutamine and increased preload. Another strategy adopted by anaesthesiologist to limit this hypotension is by reducing isoflurane and thus cardiac surgical patients are prone for awareness. Awareness is the explicit recall of sensory perceptions during anaesthesia.METHODSWe studied 40 patients with ASA physical status II & III, between age group of 18 to 65 years scheduled for elective off pump CABG after institutional ethical committee clearance and written informed consent. Patients were randomly allocated into two groups of 20 each. Group 1 (isoflurane in oxygen given with BIS maintained at 55+/-5) and Group 2 (isoflurane in oxygen given without BIS).Comparison of the two groups was done in terms of gender, age, height, weight, heart rate, hemodynamics, dial concentration, minimum alveolar concentration, drugs consumed, time to extubation and intraoperative awareness. Results were statistically analyzed using independent t test, chi square test and Fischer exact test. Data was presented in terms of mean, median and standard deviation. The 'p' value of <0.05 was considered significant.RESULTSHeart rate, systolic blood pressure, diastolic blood pressure and mean arterial pressure were higher in Group 1 compared to Group 2. The dial concentration and minimum alveolar concentration were found to be statistically significant 5 minutes after intubation upto 4.5 hours of the cardiac surgical procedure with 'p' value <0.05. Amount of midazolam and propofol used in Group 1 was higher when compared to Group 2 while there was no statistical significance with use of opioid (fentanyl) or muscle relaxant (pancuronium). Time to extubation and intraoperative awareness were comparable between both the groups.CONCLUSIONSBIS monitoring reduces amount of isoflurane used along with the prevention of awareness in cardiac surgical patients. It helps not only the anaesthesiologist but also the other operation theatre personnel by preventing environmental pollution.

In silico and in vitro assay of Hexagamavunon-6 analogs, Dibenzilyden-N-Methyl-4-piperidone as antibacterial agents

A new series of analogs Hexagamavunon-6 (HGV-6) was prepared and screened for antibacterial activity againstStreptococcus mutans (ATCC 25175), Escherichia coli (ATCC 25922), Bacillus subtilis (ATCC 6633), Psedomonasaeruginosa (ATCC 27853), Klebsiella pneumoniae, and Enterococcus faecalis (ATCC 29212) using disk diffusionmethod. The antibacterial results showed that 3,5-Bis-(2',4'-dichlorobenzilyden)-N-methyl-4-piperidone (1c)compound display significant inhibition and broad-spectrum antibacterial activity. This is in accordance with the insilico evaluation showing that compound 1c has a lower docking score than both compounds 1a and 1b. None of thetested compounds were as active as the reference standard drug Amoxicillin.

Response of bisphosphonate therapy in recurrent tumoral calcinosis

Tumoral calcinosis is a rare condition characterized by solitary or multiple, periarticular masses. Surgical excision of the tumoral calcinosis lesion is a well-documented treatment, but recurrences are not uncommon. A case of 42 year old male patient of tumoral calcinosis presented to us with history of repeated surgical excision twice in past 8 years for recurrent swellings. He was started on IV zoledronic acid and the patient has shown improvement after two years with no recurrence in follow up.

Preliminary observation on imbalance degree of impedance in extracellular fluid of cells in the twelve meridians in healthy subjects / 中国针灸

OBJECTIVE@#To calculate the imbalance degree (IBD) of left-right meridian (IBD-LRM), IBD of exterior-interior meridian (IBD-EIM) and IBD of hand-foot meridians (IBD-HFM) of impedance in extracellular fluid of cells in twelve meridians of healthy subjects, so as to provide foundation for meridian diagnosis.@*METHODS@#A total of 31 healthy volunteers were enrolled and bioelectrical impedance spectroscopy (BIS) was applied. The constant current (from 1 to 100 kHz, 200 μA) was connected into the bilateral twelve meridians through two excitation electrodes with a distance of 10 cm. Two measuring electrodes, with an interval of 5 cm, were set in between the two excitation electrodes to collect the voltage amplitude and phase. The Cole-Cole curve fitting was used to calculate the impedance of extracellular fluid of cells in the twelve meridians; the IBD-LRM, IBD-EIM and IBD-HFM as well as their absolute values were calculated.@*RESULTS@#The impedance of extracellular fluid in the left side was higher than that in right side in the large intestine meridian, the small intestine meridian and the bladder meridian (<0.05, <0.01). The mean value of IBD-LRM of extracellular fluid was (4.0±1.4) %; the mean value of absolute value of IBD-LRM was (15.0±1.1) %; the maximum absolute value of IBD-LRM was the bladder meridian. The mean value of IBD-EIM was (3.3±1.0) %; the mean value of absolute value of IBD-EIM was (17.9±1.6) %; the maximum absolute value of IBD-EIM was the bladder meridian and the kidney meridian. The impedance of extracellular fluid of hand meridian, hand meridian and hand meridian were lower than those of foot meridians. The mean value of IBD-HFM was (-2.6±1.1) %; the mean value of absolute value of IBD-HFM was (19.7±1.7) %; the maximum absolute value of IBD-HFM was meridian; the imbalance of meridians was greater than meridians. There were significant differences in impedance of extracellular fluid between left and right and between hands and feet (<0.05, <0.01).@*CONCLUSION@#The extracellular fluid of left-right meridians of healthy subjects is different, but the absolute value of IBD is low; the mean value of exterior meridian and interior meridian is very close, and the absolute value of IBD is medium; the impedance of the foot meridians are greater than the hand meridians, and the absolute value of IBD is relatively high.

Neuroprotective effects of bis(7)-tacrine in rat model with glaucoma / 国际眼科杂志(Guoji Yanke Zazhi)

@#AIM: To assess the neuroprotective effect of bis(7)-tacrine in experimental Sprague-Dawley(SD)rat glaucoma.<p>METHODS: Totally 24 rats were randomly divided into control group, operated group, 0.5mg/kg bis(7)-tacrine group and 5mg/kg memantine group. Unilateral elevation of intraocular pressure(IOP)was produced by hypertonic saline injection into an episcleral vein. Animals were orally dosed daily with bis(7)-tacrine or memantine. IOP was measured in both eyes of animals per 3d, and the number of retinal ganglion cells and the thickness of nerve fiber layer axon bundle were measured at 5wk.<p>RESULTS: Elevated IOP were induced in 3 glaucoma groups. Compared with control group, the retinal ganglion cells decreased from 119.50±8.26 to 79.83±9.58 and the thickness of axon bundle come down from 13.40±0.60 μm to 6.64±0.50 μm in operated group. However the number of the retinal ganglion cells was 109.00±7.04 in bis(7)-tacrine group and 107.33±8.57 in memantine group individually. The thickness of axon bundle was 12.26±0.78μm in bis(7)-tacrine group and 10.13±1.19μm in memantine group individually.<p>CONCLUSION: Both bis(7)-tacrine and memantine inhibited retinal ganglion cells loss, but only bis(7)-tacrine decreased the thickness declining of axon bundle.